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本研究设计了一条新的路线合成酮基布洛芬(1)。1-(4-硝基苯)丙-1-酮(2)经乙二醇保护得2-乙基-2-(4-硝基苯基)-1,3-二氧戊环(3),再与苯乙腈成环,然后在铁/盐酸作用下还原开环得1-(4-氨基-3-苯甲酰基苯)丙-1-酮(4),4经重氮化去氨基、再经溴化生成1-(3-苯甲酰基苯基)-2-溴丙酮(6),6与新戊二醇反应后,在乙酸钾作用下重排成酯,再经水解得1,总收率40%(以2计)。本工艺反应条件温和,后处理简便,易于量产。其中,4为未见文献报道的新化合物。
This study designed a new route for the synthesis of ketoprofen (1). 1- (4-nitrophenyl) propan-1-one (2) Ethylene glycol protected 2-ethyl-2- , And then with benzene acetonitrile into ring, and then under the action of iron / hydrochloric acid to open the ring was 1- (4-amino-3-benzoylbenzene) propan-1-one (4), 4 diazotization deaminated, After bromination to generate 1- (3-benzoylphenyl) -2-bromoacetone (6), 6 with neopentyl glycol after the role of potassium acetate rearranged into esters, and then by hydrolysis 1, The total yield of 40% (2). The reaction conditions mild, post-processing simple, easy mass production. Among them, 4 are new compounds which have not been reported in the literature.